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The novel antagonist, S33084, and GR218,231 interact selectively with cloned and native, rat dopamine D3 receptors as compared with native, rat dopamine D2 receptors.

Cussac D, Newman-Tancredi A, Sezgin L, Millan MJ.
Eur J Pharmacol. 2000 Apr 7;394(1):47-50.

The novel benzopyranopyrrole, S33084 ((3aR,9bS)-N[4-(8-cyano-1,3a,4, 9b-tetrahydro-3H-benzopyrano[3,4-c]pyrrole-2-yl)-butyl] (4-phenyl)benzamide)), and the aminotetralin derivative, GR218,231 (2(R,S)-(di-n-propylamino)-6-(4-methoxyphenylsulfonylmethyl)-1,2,3 , 4-tetrahydro naphthalene), displayed high affinity at cloned, rat dopamine D3 receptors (pKis of 8.72 and 8.67, respectively), as well as dopamine D3 receptors in rat olfactory tubercle (8.62 and 8.94, respectively). In contrast, they showed low affinities at striatal dopamine D2 receptors (6.82 and 6.64, respectively). Unlike S33084 and GR218,231, the arylpiperazine, L741,626 (4-(4-chlorophenyl)-1-(1H-indol-3-ylmethyl)piperidin-4-ol), showed lower affinity for cloned (6.46) and native (6.92) dopamine D3 receptors than for striatal dopamine D2 receptors (7.52). S33084, GR218,231 and L741,626 should prove useful tools for exploration of the functional roles of dopamine D3 vs. dopamine D2 receptors.